EP1904457A4 - Compositions and methods for inhibition of the jak pathway - Google Patents

Compositions and methods for inhibition of the jak pathway

Info

Publication number
EP1904457A4
EP1904457A4 EP06784727A EP06784727A EP1904457A4 EP 1904457 A4 EP1904457 A4 EP 1904457A4 EP 06784727 A EP06784727 A EP 06784727A EP 06784727 A EP06784727 A EP 06784727A EP 1904457 A4 EP1904457 A4 EP 1904457A4
Authority
EP
European Patent Office
Prior art keywords
inhibition
compositions
methods
jak pathway
jak
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP06784727A
Other languages
German (de)
French (fr)
Other versions
EP1904457B1 (en
EP1904457A2 (en
Inventor
Hui Li
Sambaiah Thota
David Carroll
Ankush Argade
Kin Tso
Arvinder Sran
Jeffrey Clough
Holger Keim
Somasekhar Bhamidipati
Vanessa Taylor
Robin Cooper
Rajinder Singh
Brian Wong
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Rigel Pharmaceuticals Inc
Original Assignee
Rigel Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Rigel Pharmaceuticals Inc filed Critical Rigel Pharmaceuticals Inc
Publication of EP1904457A2 publication Critical patent/EP1904457A2/en
Publication of EP1904457A4 publication Critical patent/EP1904457A4/en
Application granted granted Critical
Publication of EP1904457B1 publication Critical patent/EP1904457B1/en
Not-in-force legal-status Critical Current
Anticipated expiration legal-status Critical

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • A61K38/13—Cyclosporins
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
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    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
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    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/0803—Compounds with Si-C or Si-Si linkages
    • C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
    • C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
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    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/15—Six-membered rings
    • C07D285/16—Thiadiazines; Hydrogenated thiadiazines
    • C07D285/18—1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines
    • C07D285/20—1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines condensed with carbocyclic rings or ring systems
    • C07D285/22—1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring

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  • Chemical & Material Sciences (AREA)
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  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
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  • Mycology (AREA)
  • Transplantation (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
EP06784727.7A 2005-06-08 2006-06-08 Compositions and methods for inhibition of the jak pathway Not-in-force EP1904457B1 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US68903205P 2005-06-08 2005-06-08
US70663805P 2005-08-08 2005-08-08
US77663606P 2006-02-24 2006-02-24
PCT/US2006/022590 WO2006133426A2 (en) 2005-06-08 2006-06-08 Compositions and methods for inhibition of the jak pathway

Publications (3)

Publication Number Publication Date
EP1904457A2 EP1904457A2 (en) 2008-04-02
EP1904457A4 true EP1904457A4 (en) 2010-06-02
EP1904457B1 EP1904457B1 (en) 2017-09-06

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EP06784727.7A Not-in-force EP1904457B1 (en) 2005-06-08 2006-06-08 Compositions and methods for inhibition of the jak pathway

Country Status (16)

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US (9) US7491732B2 (en)
EP (1) EP1904457B1 (en)
JP (2) JP5225079B2 (en)
KR (1) KR101312225B1 (en)
CN (1) CN105348203B (en)
AU (1) AU2006254840B2 (en)
BR (1) BRPI0610876B8 (en)
CA (1) CA2608367C (en)
ES (1) ES2651349T3 (en)
IL (1) IL187257A (en)
MX (1) MX286273B (en)
NO (1) NO341966B1 (en)
NZ (1) NZ563454A (en)
RU (1) RU2485106C2 (en)
SG (1) SG137989A1 (en)
WO (1) WO2006133426A2 (en)

Families Citing this family (135)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI329105B (en) * 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
CN1678321A (en) 2002-07-29 2005-10-05 里格尔药品股份有限公司 Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
EP1656372B1 (en) * 2003-07-30 2013-04-10 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
US7557207B2 (en) 2004-11-24 2009-07-07 Rigel Pharmaceuticals, Inc. Spiro 2,4-pyrimidinediamine compounds and their uses
PT1856135E (en) 2005-01-19 2010-02-26 Rigel Pharmaceuticals Inc Prodrugs of 2,4-pyrimidinediamine compounds and their uses
SG137989A1 (en) 2005-06-08 2008-01-28 Rigel Pharmaceuticals Inc Compositions and methods for inhibition of the JAK pathway
US20070203161A1 (en) * 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
CA2607901C (en) 2005-06-13 2016-08-16 Rigel Pharmaceuticals, Inc. Methods and compositions for treating degenerative bone disorders using a syk inhibitory 2,4-pyrimidinediamine
MY167260A (en) * 2005-11-01 2018-08-14 Targegen Inc Bi-aryl meta-pyrimidine inhibitors of kinases
US8133900B2 (en) 2005-11-01 2012-03-13 Targegen, Inc. Use of bi-aryl meta-pyrimidine inhibitors of kinases
US8604042B2 (en) 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
US7713987B2 (en) * 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
ES2970354T3 (en) 2005-12-13 2024-05-28 Incyte Holdings Corp Pyrrolo[2,3-d]pyrimidine derivatives as Janus kinase inhibitors
SI1984357T1 (en) * 2006-02-17 2014-02-28 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for treating or preventing autoimmune diseases
CA2642229C (en) * 2006-02-24 2015-05-12 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
WO2007146981A2 (en) 2006-06-15 2007-12-21 Boehringer Ingelheim International Gmbh 2-anilino-4-(heterocyclic)amino-pyrimidines as inhibitors of protein kinase c-alpha
CA2673125C (en) 2006-10-19 2015-04-21 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
CN101535276B (en) 2006-10-23 2013-08-28 赛福伦公司 Fused bicyclic derivatives of 2,4-diaminopyrimidine as ALK and c-MET inhibitors
CA2673137C (en) 2006-11-21 2015-02-10 Rigel Pharmaceuticals, Inc. Prodrug salts of 2,4-pyrimidinediamine compounds and their uses
RS53588B1 (en) 2006-12-08 2015-02-27 Irm Llc Compounds and compositions as protein kinase inhibitors
US7947698B2 (en) * 2007-03-23 2011-05-24 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
WO2008118823A2 (en) * 2007-03-26 2008-10-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US20090036440A1 (en) * 2007-04-27 2009-02-05 Astrazeneca Ab Novel pyrimidine derivatives - 816
TR201903488T4 (en) 2007-06-13 2019-04-22 Incyte Holdings Corp Use of Janus kinase inhibitor (r) -3- (4- (7h-pyrrolo [2,3-d] pyrimidin-4-yl) -1h-pyrazol-1-yl) -3-cyclopentylpropannitrile salts.
EP2183225A1 (en) 2007-07-17 2010-05-12 Rigel Pharmaceuticals, Inc. Cyclic amine substituted pyrimidinediamines as pkc inhibitors
FR2919869B1 (en) * 2007-08-09 2009-09-25 Sanofi Aventis Sa NOVEL N, N'-2,4-DIANILINOPYRIMIDINE DERIVATIVES, THEIR PREPARATION AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS AND IN PARTICULAR AS INHIBITORS OF IKK
WO2009109991A2 (en) * 2008-01-23 2009-09-11 Sun Pharma Advanced Research Company Ltd., Novel hydrazide containing tyrosine kinase inhibitors
EA029131B1 (en) 2008-05-21 2018-02-28 Ариад Фармасьютикалз, Инк. Phosphorous derivatives as kinase inhibitors
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
SG178807A1 (en) 2008-06-20 2012-03-29 Genentech Inc Triazolopyridine jak inhibitor compounds and methods
BRPI0910021A2 (en) 2008-06-20 2015-09-01 Genentech Inc "compound, pharmaceutical composition, method for treating or alleviating the severity of a disease or condition responsive to inhibition of jak2 kinase activity in a patient, kit for treating a disease or disorder responsive to inhibition of jak kinase"
MX2010014029A (en) * 2008-06-27 2011-01-21 Avila Therapeutics Inc Heteroaryl compounds and uses thereof.
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
US11351168B1 (en) 2008-06-27 2022-06-07 Celgene Car Llc 2,4-disubstituted pyrimidines useful as kinase inhibitors
EP2341052A4 (en) * 2008-09-05 2011-10-12 Shionogi & Co Ring-fused morpholine derivative having pi3k-inhibiting activity
EP2334301B1 (en) * 2008-09-08 2018-02-14 Merck Serono SA Macrocyclics pyrimidines as aurora kinase inhibitors
JP5518076B2 (en) * 2008-09-23 2014-06-11 ライジェル ファーマシューティカルズ， インコーポレイテッド Tricyclic carbamate JAK inhibitor
CL2009001884A1 (en) * 2008-10-02 2010-05-14 Incyte Holdings Corp Use of 3-cyclopentyl-3- [4- (7h-pyrrolo [2,3-d] pyrimidin-4-yl) -1h-pyrazol-1-yl) propanonitrile, janus kinase inhibitor, and use of a composition that understands it for the treatment of dry eye.
WO2010061971A1 (en) 2008-11-28 2010-06-03 興和株式会社 Pyridine-3-carboxyamide derivative
US8809343B2 (en) * 2008-12-26 2014-08-19 Fudan University Pyrimidine derivative, preparation method and use thereof
CN102292333B (en) * 2009-01-15 2015-05-13 里格尔药品股份有限公司 Protein kinase c inhibitors and uses thereof
PT2565193E (en) 2009-01-23 2014-06-05 Rigel Pharmaceuticals Inc Compositions and methods for inhibition of the jak pathway
KR101705158B1 (en) 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Egfr inhibitors and methods of treating diseases
KR101771401B1 (en) 2009-05-22 2017-08-25 인사이트 홀딩스 코포레이션 N-(HETERO)ARYL-PYRROLIDINE DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AND PYRROL-3-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS
TWI484962B (en) 2009-05-22 2015-05-21 Incyte Corp 3-(4-(7h-pyrrolo(2,3-d)pyrimidin-4-yl)-1h-pyrazol-1-yl)octane-or heptane-nitrile as jak inhibitors
WO2010144468A1 (en) 2009-06-10 2010-12-16 Abbott Laboratories 2- ( lh-pyrazol-4 -ylamino ) -pyrimidine as kinase inhibitors
BR112012002001A2 (en) 2009-07-28 2016-05-10 Rigel Pharmaceuticals Inc method for treating an eye disease and / or disorder, pharmaceutical formulation, and kit
US9249145B2 (en) 2009-09-01 2016-02-02 Incyte Holdings Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
CA2776028C (en) 2009-10-15 2015-12-01 Pfizer Inc. Pyrrolo[2,3-d]pyrimidine compounds
JP5739446B2 (en) 2009-12-18 2015-06-24 ファイザー・インク Pyrrolo [2,3-d] pyrimidine compound
WO2011100455A1 (en) 2010-02-12 2011-08-18 The Government Of The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Inhibition of antibody responses to foreign proteins
DK2545045T3 (en) 2010-03-10 2016-01-25 Incyte Holdings Corp PIPERIDINE-4-YL-azetidine derivatives AS JAK1 INHIBITORS
AU2011255218B2 (en) 2010-05-21 2015-03-12 Infinity Pharmaceuticals, Inc. Chemical compounds, compositions and methods for kinase modulation
CN103002875B (en) 2010-05-21 2016-05-04 因塞特控股公司 Topical formulations of JAK inhibitors
EP2395001A1 (en) 2010-05-21 2011-12-14 Chemilia AB Novel pyrimidine derivatives
RU2528386C2 (en) 2010-05-21 2014-09-20 Кемилиа Аб New pyrimidine derivatives
RS54865B1 (en) 2010-06-04 2016-10-31 Hoffmann La Roche Aminopyrimidine derivatives as lrrk2 modulators
US8710223B2 (en) 2010-07-21 2014-04-29 Rigel Pharmaceuticals, Inc. Protein kinase C inhibitors and uses thereof
MX336875B (en) 2010-08-10 2016-02-04 Celgene Avilomics Res Inc Besylate salt of a btk inhibitor.
JP5956999B2 (en) 2010-11-01 2016-07-27 セルジーン アヴィロミクス リサーチ， インコーポレイテッド Heteroaryl compounds and uses thereof
SG10201508958WA (en) 2010-11-01 2015-11-27 Celgene Avilomics Res Inc Heterocyclic Compounds And Uses Thereof
US9198911B2 (en) 2010-11-02 2015-12-01 The Trustees Of Columbia University In The City Of New York Methods for treating hair loss disorders
CA2816957A1 (en) 2010-11-07 2012-05-10 Targegen, Inc. Compositions and methods for treating myelofibrosis
SG189043A1 (en) 2010-11-10 2013-05-31 Hoffmann La Roche Pyrazole aminopyrimidine derivatives as lrrk2 modulators
JP5957003B2 (en) 2010-11-10 2016-07-27 セルジーン アヴィロミクス リサーチ， インコーポレイテッド Mutant selective EGFR inhibitor and use thereof
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
US8933085B2 (en) 2010-11-19 2015-01-13 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
RS57672B1 (en) * 2011-03-10 2018-11-30 Rigel Pharmaceuticals Inc 2,4 substituted pyrimidinediamines for use in discoid lupus
ES2587864T3 (en) 2011-03-24 2016-10-27 Noviga Research Ab Pyrimidine derivatives
EP2502924A1 (en) 2011-03-24 2012-09-26 Chemilia AB Novel pyrimidine derivatives
US9834518B2 (en) 2011-05-04 2017-12-05 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in EGFR-driven cancers
US9145391B2 (en) 2011-05-10 2015-09-29 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as Syk inhibitors
WO2012154519A1 (en) 2011-05-10 2012-11-15 Merck Sharp & Dohme Corp. Aminopyrimidines as syk inhibitors
CA2834062A1 (en) 2011-05-10 2012-11-15 Merck Sharp & Dohme Corp. Pyridyl aminopyridines as syk inhibitors
MX344479B (en) 2011-06-20 2016-12-16 Incyte Holdings Corp Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors.
TW201313721A (en) 2011-08-18 2013-04-01 Incyte Corp Cyclohexyl azetidine derivatives as JAK inhibitors
CA2846431A1 (en) 2011-08-29 2013-03-07 Infinity Pharmaceuticals Inc. Heterocyclic compounds and uses thereof
UA111854C2 (en) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн METHODS AND INTERMEDIATE COMPOUNDS FOR JAK INHIBITORS
EP2763976B1 (en) 2011-10-05 2016-05-18 Merck Sharp & Dohme Corp. 2-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
EP2763974B1 (en) 2011-10-05 2016-09-14 Merck Sharp & Dohme Corp. Phenyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
WO2013052393A1 (en) 2011-10-05 2013-04-11 Merck Sharp & Dohme Corp. 3-PYRIDYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS
WO2013063401A1 (en) 2011-10-28 2013-05-02 Celgene Avilomics Research, Inc. Methods of treating a bruton's tyrosine kinase disease or disorder
JP6247223B2 (en) * 2011-12-08 2017-12-13 ライジェル ファーマシューティカルズ， インコーポレイテッド Topical formulations for administering compounds
KR102090453B1 (en) 2012-03-15 2020-03-19 셀젠 카르 엘엘씨 Salts of an epidermal growth factor receptor kinase inhibitor
BR112014022789B1 (en) 2012-03-15 2022-04-19 Celgene Car Llc Solid forms of an epidermal growth factor receptor kinase inhibitor, pharmaceutical composition and uses thereof
WO2013169401A1 (en) 2012-05-05 2013-11-14 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
AR091079A1 (en) 2012-05-18 2014-12-30 Incyte Corp DERIVATIVES OF PIRROLOPIRIMIDINA AND PIRROLOPIRIDINA REPLACED WITH PIPERIDINILCICLOBUTILO AS JAK INHIBITORS
EP2863913B1 (en) 2012-06-20 2018-09-12 Merck Sharp & Dohme Corp. Imidazolyl analogs as syk inhibitors
US9242984B2 (en) 2012-06-20 2016-01-26 Merck Sharp & Dohme Corp. Pyrazolyl derivatives as Syk inhibitors
EP2863915B1 (en) 2012-06-22 2017-12-06 Merck Sharp & Dohme Corp. SUBSTITUTED DIAZINE AND TRIAZINE SPLEEN TYROSINE KINASE (Syk) INHIBITORS
WO2013192098A1 (en) 2012-06-22 2013-12-27 Merck Sharp & Dohme Corp. SUBSTITUTED PYRIDINE SPLEEN TYROSINE KINASE (Syk) INHIBITORS
WO2014031438A2 (en) 2012-08-20 2014-02-27 Merck Sharp & Dohme Corp. SUBSTITUTED PHENYL SPLEEN TYROSINE KINASE (Syk) INHIBITORS
JP2015528501A (en) 2012-09-12 2015-09-28 ライジェル ファーマシューティカルズ， インコーポレイテッド Treatment of vitiligo
EP2711365A1 (en) 2012-09-21 2014-03-26 Chemilia AB 4-Indazolylamino-2-(2-(indol-3-yl)ethyl)aminopyrimidines useful for the treatment of cancer
EP2711364A1 (en) 2012-09-21 2014-03-26 Chemilia AB 4-(Indolyl or benzimidazolyl)amino-2-(2-(indol-3-yl)ethyl)aminopyrimidines useful for the treatment of cancer
WO2014048065A1 (en) 2012-09-28 2014-04-03 Merck Sharp & Dohme Corp. Triazolyl derivatives as syk inhibitors
KR20210037012A (en) 2012-11-15 2021-04-05 인사이트 홀딩스 코포레이션 Sustained-release dosage forms of ruxolitinib
EP2931281B1 (en) 2012-12-12 2018-01-17 Merck Sharp & Dohme Corp. Amino-pyrimidine-containing spleen tyrosine kinase inhibitors
EP2934525B1 (en) 2012-12-21 2019-05-08 Merck Sharp & Dohme Corp. Thiazole-substituted aminopyridines as spleen tyrosine kinase inhibitors
WO2014100748A1 (en) 2012-12-21 2014-06-26 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
CA2900012A1 (en) 2013-02-08 2014-08-14 Celgene Avilomics Research, Inc. Erk inhibitors and uses thereof
CA2903418C (en) 2013-03-06 2021-03-23 Incyte Corporation Processes and intermediates for making a jak inhibitor
US9481667B2 (en) 2013-03-15 2016-11-01 Infinity Pharmaceuticals, Inc. Salts and solid forms of isoquinolinones and composition comprising and methods of using the same
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
EP2988749B1 (en) 2013-04-26 2019-08-14 Merck Sharp & Dohme Corp. Thiazole-substituted aminopyrimidines as spleen tyrosine kinase inhibitors
EP2988744A4 (en) 2013-04-26 2016-11-02 Merck Sharp & Dohme Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
BR122020001831A8 (en) 2013-08-07 2023-01-24 Incyte Corp {1-{1-[3-FLUORINE-2-(TRIFLUORMETHYL)ISONICOTINOL]PIPERIDIN-4-IL}-3-[4-(7H-PYROLO[2,3-D]PRIMIDIN-4-IL) -1H- PYRAZOL-1-YL]AZETIDIN-3-YL}ACETONITRIL, ITS USE, SUSTAINED RELEASE DOSAGE FORMS AND DOSES
US9492471B2 (en) 2013-08-27 2016-11-15 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase
EP3059227B1 (en) 2013-10-16 2019-06-26 FUJIFILM Corporation Salt of nitrogen-containing heterocyclic compound or crystal thereof, pharmaceutical composition, and flt3 inhibitor
US9783531B2 (en) 2013-12-20 2017-10-10 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
US9822107B2 (en) 2013-12-20 2017-11-21 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
US9670196B2 (en) 2013-12-20 2017-06-06 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as Spleen Tyrosine Kinase inhibitors
US9415049B2 (en) 2013-12-20 2016-08-16 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
US10793571B2 (en) 2014-01-31 2020-10-06 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
CA2936865A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Diaminopyrimidine benzenesulfone derivatives and uses thereof
US9775839B2 (en) 2014-03-13 2017-10-03 Merck Sharp & Dohme Corp. 2-pyrazine carboxamides as spleen tyrosine kinase inhibitors
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
WO2016022902A1 (en) 2014-08-08 2016-02-11 Dana-Farber Cancer Institute, Inc. Diazepane derivatives and uses thereof
WO2016025561A1 (en) 2014-08-13 2016-02-18 Celgene Avilomics Research, Inc. Forms and compositions of an erk inhibitor
BR112017003186A2 (en) 2014-08-22 2017-11-28 Fujifilm Corp pharmaceutical composition for treatment of positive cancer for mutation in flt3, mutant flt3 inhibitor and uses thereof
AU2016276963C1 (en) 2015-06-12 2021-08-05 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
JP6412471B2 (en) 2015-07-15 2018-10-24 富士フイルム株式会社 Process for producing nitrogen-containing heterocyclic compound and intermediate thereof
MX2018003031A (en) 2015-09-11 2018-08-01 Dana Farber Cancer Inst Inc Cyano thienotriazolodiazepines and uses thereof.
KR20180051576A (en) 2015-09-11 2018-05-16 다나-파버 캔서 인스티튜트 인크. Acetamide thienotriazolol diazepines and their uses
SG11201803210YA (en) 2015-11-25 2018-05-30 Dana Farber Cancer Inst Inc Bivalent bromodomain inhibitors and uses thereof
JP6999688B2 (en) * 2016-12-13 2022-02-10 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Novel 6-aminoquinolinone compounds and derivatives as BCL6 inhibitors
JOP20180094A1 (en) 2017-10-18 2019-04-18 Hk Inno N Corp Heterocyclic compound as a protein kinase inhibito
CN107805212B (en) * 2017-11-03 2021-08-20 宿迁德威化工股份有限公司 Preparation method of 2-methyl-5-aminobenzenesulfonamide
AR113922A1 (en) 2017-12-08 2020-07-01 Incyte Corp LOW DOSE COMBINATION THERAPY FOR THE TREATMENT OF MYELOPROLIFERATIVE NEOPLASMS
CN112105608B (en) 2018-01-30 2023-07-14 因赛特公司 Process for the preparation of (1- (3-fluoro-2- (trifluoromethyl) isonicotinyl) piperidin-4-one
US11304949B2 (en) 2018-03-30 2022-04-19 Incyte Corporation Treatment of hidradenitis suppurativa using JAK inhibitors
CN114698370A (en) 2019-08-08 2022-07-01 里格尔药品股份有限公司 Compounds and methods for treating cytokine release syndrome
AU2020385527B2 (en) * 2019-11-21 2023-04-13 Tyk Medicines, Inc. Compound used as EGFR kinase inhibitor and use thereof
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
US11773084B1 (en) * 2023-04-14 2023-10-03 King Faisal University 4-arylamino-2-(6-indolylamino)pyrimidine compounds as antibacterial agents

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001064654A1 (en) * 2000-03-01 2001-09-07 Astrazeneca Ab Pyrimidine compounds
WO2002004429A1 (en) * 2000-07-11 2002-01-17 Astrazeneca Ab Pyrimidine derivatives
WO2004041810A1 (en) * 2002-11-05 2004-05-21 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of jak and other protein kinases
WO2004041789A1 (en) * 2002-11-01 2004-05-21 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of jak and other protein kinases
WO2005012307A1 (en) * 2003-07-16 2005-02-10 Janssen Pharmaceutica N.V. Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors
WO2005012294A1 (en) * 2003-07-30 2005-02-10 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
WO2005013996A2 (en) * 2003-08-07 2005-02-17 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and uses as anti-proliferative agents
WO2005026130A1 (en) * 2003-09-18 2005-03-24 Novartis Ag 2,4-di (phenylamino) pyrimidines useful in the treatment of proliferative disorders
WO2006034872A1 (en) * 2004-09-29 2006-04-06 Bayer Schering Pharma Aktiengesellschaft Substituted 2-anilinopyrimidines as cell cycle kinase inhibitors or receptor tyrosine kinase inhibitors, production of said substances and use of the latter as medicaments

Family Cites Families (160)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4166452A (en) 1976-05-03 1979-09-04 Generales Constantine D J Jr Apparatus for testing human responses to stimuli
US4256108A (en) 1977-04-07 1981-03-17 Alza Corporation Microporous-semipermeable laminated osmotic system
US4166542A (en) * 1977-12-05 1979-09-04 Bryan John F Jr Telescoping lattice boom crane
US4265874A (en) 1980-04-25 1981-05-05 Alza Corporation Method of delivering drug with aid of effervescent activity generated in environment of use
CN87210811U (en) 1987-07-25 1988-04-20 徐正斌 Handy drug feeding box
US5728536A (en) 1993-07-29 1998-03-17 St. Jude Children's Research Hospital Jak kinases and regulation of Cytokine signal transduction
CZ101496A3 (en) 1993-10-12 1996-11-13 Du Pont Merck Pharma N-alkyl-n-aryl-pyrimidinamines and derivatives thereof
US5700904A (en) 1995-06-07 1997-12-23 Eli Lilly And Company Preparation of an acylated protein powder
US6316635B1 (en) 1995-06-07 2001-11-13 Sugen, Inc. 2-indolinone derivatives as modulators of protein kinase activity
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
US6696448B2 (en) 1996-06-05 2004-02-24 Sugen, Inc. 3-(piperazinylbenzylidenyl)-2-indolinone compounds and derivatives as protein tyrosine kinase inhibitors
JPH10271051A (en) 1997-03-11 1998-10-09 Alcatel Alsthom Co General Electricite Transmitter-receiver with two-way equalization
US6316429B1 (en) 1997-05-07 2001-11-13 Sugen, Inc. Bicyclic protein kinase inhibitors
US6486185B1 (en) 1997-05-07 2002-11-26 Sugen, Inc. 3-heteroarylidene-2-indolinone protein kinase inhibitors
GB9718913D0 (en) 1997-09-05 1997-11-12 Glaxo Group Ltd Substituted oxindole derivatives
US6133305A (en) 1997-09-26 2000-10-17 Sugen, Inc. 3-(substituted)-2-indolinones compounds and use thereof as inhibitors of protein kinase activity
NZ506417A (en) 1998-02-17 2003-05-30 Tularik Inc Anti-viral pyrimidine derivatives
JP2004504259A (en) 1998-06-30 2004-02-12 パーカー　ヒューズ　インスティテュート Method of inhibiting C-JUN expression using JAK-3 inhibitor
MXPA01001893A (en) 1998-08-21 2002-04-24 Parker Hughes Inst Quinazoline derivatives.
JP2002523497A (en) 1998-08-29 2002-07-30 アストラゼネカ・アクチエボラーグ Pyrimidine compounds
UA70966C2 (en) 1998-11-10 2004-11-15 Янссен Фармацевтика Н.В. Pirimidines inhibiting hiv replication
GB9828511D0 (en) 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
US6841567B1 (en) 1999-02-12 2005-01-11 Cephalon, Inc. Cyclic substituted fused pyrrolocarbazoles and isoindolones
GB9904995D0 (en) 1999-03-04 1999-04-28 Glaxo Group Ltd Substituted aza-oxindole derivatives
US6624171B1 (en) 1999-03-04 2003-09-23 Smithkline Beecham Corporation Substituted aza-oxindole derivatives
US6080747A (en) 1999-03-05 2000-06-27 Hughes Institute JAK-3 inhibitors for treating allergic disorders
US7125875B2 (en) 1999-04-15 2006-10-24 Bristol-Myers Squibb Company Cyclic protein tyrosine kinase inhibitors
GB9914258D0 (en) 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
CA2392554A1 (en) 1999-11-30 2001-06-28 Parker Hughes Institute Inhibitors of thrombin induced platelet aggregation
PT1235830E (en) 1999-12-10 2004-04-30 Pfizer Prod Inc PYRIMIDINE-2,3-D | PYRIMIDINE COMPOUNDS AS PROTEIN KINASE INHIBITORS
ES2245955T3 (en) 1999-12-21 2006-02-01 Sugen, Inc. 7-AZA-INDOLIN-2-ONAS 4-SUBSTITUTES AND THEIR USE AS PROTEIN-KINASE INHIBITORS.
US20020065270A1 (en) 1999-12-28 2002-05-30 Moriarty Kevin Joseph N-heterocyclic inhibitors of TNF-alpha expression
JP4794793B2 (en) 1999-12-28 2011-10-19 ファーマコペイア， インコーポレイテッド N-heterocyclic TNF-α expression inhibitor
JP5512909B2 (en) 2000-01-24 2014-06-04 ジェンザイム・コーポレーション JAK / STAT pathway inhibitors and uses thereof
DE10003668B4 (en) 2000-01-28 2005-09-15 Xion Gmbh Flexible endoscope
CA2369076A1 (en) 2000-02-05 2001-08-09 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of erk
AU782775B2 (en) 2000-02-05 2005-08-25 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of ERK
EP1257546A1 (en) 2000-02-17 2002-11-20 Amgen Inc. Kinase inhibitors
GB0004886D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004887D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
AR028261A1 (en) 2000-03-28 2003-04-30 Wyeth Corp TRICICLIC INHIBITORS OF PROTEIN QUINASA
US6608048B2 (en) 2000-03-28 2003-08-19 Wyeth Holdings Tricyclic protein kinase inhibitors
WO2001085700A2 (en) 2000-05-08 2001-11-15 Janssen Pharmaceutica N.V. Hiv replication inhibiting pyrimidines and triazines
EP1282607B1 (en) 2000-05-08 2015-11-11 Janssen Pharmaceutica NV Prodrugs of hiv replication inhibiting pyrimidines
SI1294724T1 (en) 2000-06-26 2006-08-31 Pfizer Prod Inc Pyrrolo(2,3-d) pyrimidine compounds as immunosuppressive agents
WO2002043735A1 (en) 2000-11-29 2002-06-06 Parker Hughes Institute Inhibitors of thrombin induced platelet aggregation
US20020115173A1 (en) 2000-12-11 2002-08-22 Children's Medical Center Corporation Short peptides from the 'A-region' of protein kinases which selectively modulate protein kinase activity
JP2004518669A (en) 2000-12-20 2004-06-24 スージェン・インコーポレーテッド 4-Aryl substituted indolinone
JP4160395B2 (en) 2000-12-21 2008-10-01 バーテックス ファーマシューティカルズ インコーポレイテッド Pyrazole compounds useful as protein kinase inhibitors
WO2002059110A1 (en) 2000-12-21 2002-08-01 Glaxo Group Limited Pyrimidineamines as angiogenesis modulators
AUPR279101A0 (en) 2001-01-30 2001-02-22 Cytopia Pty Ltd Protein kinase signalling
US20040102455A1 (en) 2001-01-30 2004-05-27 Burns Christopher John Method of inhibiting kinases
GB0103926D0 (en) 2001-02-17 2001-04-04 Astrazeneca Ab Chemical compounds
CN100415744C (en) 2001-02-20 2008-09-03 阿斯特拉曾尼卡有限公司 2-arylamino-pyrimidines for the treatment of GSK3-related disorders
IL159120A0 (en) 2001-05-29 2004-05-12 Schering Ag Cdk inhibiting pyrimidines, production thereof and their use as medicaments
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
EP1399440B1 (en) 2001-06-15 2009-06-03 Vertex Pharmaceuticals Incorporated 5-(2-aminopyrimidin-4-yl)benzisoxazoles as protein kinase inhibitors
EP1397142A4 (en) 2001-06-19 2004-11-03 Bristol Myers Squibb Co Pyrimidine inhibitors of phosphodiesterase (pde) 7
WO2003000186A2 (en) 2001-06-21 2003-01-03 Ariad Pharmaceuticals, Inc. Novel phenylamino-pyrimidines and uses thereof
JO3429B1 (en) 2001-08-13 2019-10-20 Janssen Pharmaceutica Nv Hiv inhibiting pyrimidines derivatives
US7115617B2 (en) 2001-08-22 2006-10-03 Amgen Inc. Amino-substituted pyrimidinyl derivatives and methods of use
US6939874B2 (en) 2001-08-22 2005-09-06 Amgen Inc. Substituted pyrimidinyl derivatives and methods of use
US6433018B1 (en) 2001-08-31 2002-08-13 The Research Foundation Of State University Of New York Method for reducing hypertrophy and ischemia
AU2002334355A1 (en) 2001-09-06 2003-03-18 Prochon Biotech Ltd. Protein tyrosine kinase inhibitors
JP2005506982A (en) 2001-09-10 2005-03-10 スージェン・インコーポレーテッド 3- (4,5,6,7-tetrahydroindol-2-ylmethylidene) -2-indolinone derivatives as kinase inhibitors
WO2003030909A1 (en) 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer
WO2003026665A1 (en) 2001-09-26 2003-04-03 Bayer Pharmaceuticals Corporation 2-phenylamino-4-(5-pyrazolylamino)-pyrimidine derivatives as kinase inhibitors, in particular, src kinase inhibitors
WO2003032994A2 (en) 2001-10-17 2003-04-24 Boehringer Ingelheim Pharma Gmbh & Co. Kg Novel tri-substituted pyrimidines, method for production and use thereof as medicament
JP4460292B2 (en) 2001-10-17 2010-05-12 ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト Pyrimidine derivatives, pharmaceutical compositions containing these compounds, their use and methods for their preparation
GT200200234A (en) 2001-12-06 2003-06-27 NEW CRYSTAL COMPOUNDS
SE0104140D0 (en) 2001-12-07 2001-12-07 Astrazeneca Ab Novel Compounds
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
US6998391B2 (en) 2002-02-07 2006-02-14 Supergen.Inc. Method for treating diseases associated with abnormal kinase activity
EP1472233A1 (en) * 2002-02-08 2004-11-03 SmithKline Beecham Corporation Pyrimidine compounds
EP1487824B1 (en) 2002-03-01 2007-06-20 SmithKline Beecham Corporation Diamino-pyrimidines and their use as angiogenesis inhibitors
US7288547B2 (en) 2002-03-11 2007-10-30 Schering Ag CDK-inhibitory 2-heteroaryl-pyrimidines, their production and use as pharmaceutical agents
JP2005526765A (en) * 2002-03-11 2005-09-08 シエーリング アクチエンゲゼルシャフト CDK-inhibiting 2-heteroaryl-pyrimidines, their production and use as pharmaceuticals
GB0206215D0 (en) 2002-03-15 2002-05-01 Novartis Ag Organic compounds
WO2003095448A1 (en) * 2002-05-06 2003-11-20 Bayer Pharmaceuticals Corporation Pyridinyl amino pyrimidine derivatives useful for treating hyper-proliferative disorders
EP2316834A1 (en) 2002-05-06 2011-05-04 Vertex Pharmaceuticals Incorporated Thiadiazoles or oxadiazoles and their use as inhibitors of JAK protein kinase
AR039540A1 (en) 2002-05-13 2005-02-23 Tibotec Pharm Ltd MICROBICIDE COMPOUNDS WITH PIRIMIDINE OR TRIAZINE CONTENT
AU2003231880A1 (en) 2002-05-30 2003-12-19 Vertex Pharmaceuticals Incorporated Inhibitors of jak and cdk2 protein kinases
IL165286A0 (en) 2002-06-17 2005-12-18 Smithkline Beecham Corp Chemical process
US7449456B2 (en) 2002-06-28 2008-11-11 Astellas Pharma, Inc. Diaminopyrimidinecarboxamide derivative
AU2003252216A1 (en) 2002-07-17 2004-02-02 Mitsubishi Chemical Corporation Water-soluble complex dye, recording fluid, and method of recording
CN1678321A (en) 2002-07-29 2005-10-05 里格尔药品股份有限公司 Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
US7304071B2 (en) 2002-08-14 2007-12-04 Vertex Pharmaceuticals Incorporated Protein kinase inhibitors and uses thereof
AU2003258335A1 (en) * 2002-08-21 2004-03-11 Teva Pharmaceutical Industries Ltd. A method for the purification of lansoprazole
CN1684738A (en) 2002-09-20 2005-10-19 爱尔康公司 Use of cytokine synthesis inhibitors for the treatment of dry eye disorders
DE60316013T2 (en) 2002-11-04 2008-05-29 Vertex Pharmaceuticals Inc., Cambridge HETEROARYL PYRIMIDINE DERIVATIVES AS JAK INHIBITORS
KR100481130B1 (en) 2002-11-08 2005-04-07 주식회사 웨어밸리 Database System Monitoring Method Without Connecting The Database System
GB0226582D0 (en) 2002-11-14 2002-12-18 Cyclacel Ltd Anti-viral compounds
GB0226583D0 (en) 2002-11-14 2002-12-18 Cyclacel Ltd Compounds
CL2003002353A1 (en) 2002-11-15 2005-02-04 Vertex Pharma COMPOUNDS DERIVED FROM DIAMINOTRIAZOLS, INHIBITORS D ELA PROTEINA QUINASA; PHARMACEUTICAL COMPOSITION; PREPARATION PROCEDURE; AND ITS USE OF THE COMPOUND IN THE TREATMENT OF DISEASES OF ALLERGIC DISORDERS, PROLIFERATION, AUTOIMMUNES, CONDIC
JP2006508976A (en) 2002-11-21 2006-03-16 ファイザー・プロダクツ・インク 3-Amino-piperazine derivatives and production method
CA2507392A1 (en) 2002-11-26 2004-06-10 Pfizer Products Inc. Method of treatment of transplant rejection
DE60326646D1 (en) 2002-12-18 2009-04-23 Vertex Pharma BENZINE OXAZOLE DERIVATIVES PROPER AS INHIBITORS OF PROTEIN KINASES
AU2004210081B2 (en) 2003-02-07 2009-11-26 Janssen Pharmaceutica N.V. Pyrimidine derivatives for the prevention of HIV infection
CL2004000303A1 (en) 2003-02-20 2005-04-08 Tibotec Pharm Ltd COMPOUNDS DERIVED FROM PYRIMIDINS AND TRIAZINES; PREPARATION PROCESS; PHARMACEUTICAL COMPOSITION; AND ITS USE TO INHIBIT HIV REPLICATION.
ATE433447T1 (en) 2003-02-20 2009-06-15 Smithkline Beecham Corp PYRIMIIDINE COMPOUNDS
GB2398582A (en) 2003-02-20 2004-08-25 Schlumberger Holdings System and method for maintaining zonal isolation in a wellbore
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
US7547794B2 (en) 2003-04-03 2009-06-16 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
EP1618094B1 (en) 2003-04-30 2007-09-05 The Institutes for Pharmaceutical Discovery, LLC Substituted heteroaryls as inhibitors of protein tyrosine phosphatases
GB0311274D0 (en) 2003-05-16 2003-06-18 Astrazeneca Ab Chemical compounds
GB0311276D0 (en) 2003-05-16 2003-06-18 Astrazeneca Ab Chemical compounds
US7915293B2 (en) 2003-05-30 2011-03-29 Rigel Pharmaceuticals, Inc. Ubiquitin ligase inhibitors
US7979448B2 (en) 2003-06-25 2011-07-12 International Business Machines Corporation Mail and calendar tool and method
AU2004257260A1 (en) 2003-07-10 2005-01-27 Neurogen Corporation Substituted heterocyclic diarylamine analogues
EA011300B1 (en) 2003-07-16 2009-02-27 Янссен Фармацевтика Н.В. Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors
WO2005009980A1 (en) 2003-07-22 2005-02-03 Neurogen Corporation Substituted pyridin-2-ylamine analogues
JP2006528629A (en) 2003-07-24 2006-12-21 メルク　エンド　カムパニー　インコーポレーテッド Tyrosine kinase inhibitor
AU2004261484A1 (en) 2003-07-30 2005-02-10 Cyclacel Limited 2-aminophenyl-4-phenylpyrimidines as kinase inhibitors
CA2534866A1 (en) 2003-08-14 2005-02-24 Pfizer Inc. Piperazine derivatives for the treatment of hiv infections
MXPA06001759A (en) * 2003-08-15 2006-05-12 Novartis Ag 2, 4-pyrimidinediamines useful in the treatment of neoplastic diseases, inflammatory and immune system disorders.
TWI339206B (en) 2003-09-04 2011-03-21 Vertex Pharma Compositions useful as inhibitors of protein kinases
WO2005028467A1 (en) 2003-09-15 2005-03-31 Anadys Pharmaceuticals, Inc. Antibacterial 3,5-diaminopiperidine-substitute aromatic and heteroaromatic compounds
GB0321710D0 (en) 2003-09-16 2003-10-15 Novartis Ag Organic compounds
CA2535313C (en) 2003-09-25 2012-07-17 Janssen Pharmaceutica N.V. Hiv replication inhibiting purine derivatives
RS20060198A (en) 2003-10-03 2008-09-29 Pfizer Limited, Imidazopyridine substituted tropane derivatives with ccr5 receptor antagonist activ ity for the treatment of hiv and inflammation
DE10349423A1 (en) 2003-10-16 2005-06-16 Schering Ag Sulfoximine-substituted parimidines as CDK and / or VEGF inhibitors, their preparation and use as medicaments
US20080312192A1 (en) 2003-11-28 2008-12-18 Guido Bold Diaryl Urea Derivatives in the Treatment of Protein Kinase Dependent Diseases
MY141255A (en) 2003-12-11 2010-03-31 Memory Pharm Corp Phosphodiesterase 4 inhibitors, including n-substituted diarylamine analogs
EP1694652A1 (en) 2003-12-19 2006-08-30 Rigel Pharmaceuticals, Inc. Stereoisomers and stereoisomeric mixtures of 1-(2,4-pyrimidinediamino)-2-cyclopentanecarboxamide synthetic intermediates
PT1704145E (en) 2004-01-12 2012-09-04 Ym Biosciences Australia Pty Selective kinase inhibitors
GB0402653D0 (en) 2004-02-06 2004-03-10 Cyclacel Ltd Compounds
KR100645040B1 (en) 2004-02-09 2006-11-10 삼성전자주식회사 Cell array of flash memory device having source strappings
AU2005214352B2 (en) 2004-02-14 2009-11-12 Irm Llc Compounds and compositions as protein kinase inhibitors
WO2005107760A1 (en) 2004-04-30 2005-11-17 Irm Llc Compounds and compositions as inducers of keratinocyte differentiation
CA2566531A1 (en) 2004-05-18 2005-12-15 Rigel Pharmaceuticals, Inc. Cycloalkyl substituted pyrimidinediamine compounds and their uses
US7268012B2 (en) 2004-08-31 2007-09-11 Micron Technology, Inc. Methods for fabrication of thin semiconductor assemblies including redistribution layers and packages and assemblies formed thereby
CA2578349A1 (en) 2004-09-01 2006-03-16 Rigel Pharmaceuticals, Inc. Synthesis of 2,4-pyrimidinediamine compounds
US7531548B2 (en) 2004-09-30 2009-05-12 Tibotec Pharmaceuticals Ltd HIV inhibiting 5-carbo- or heterocyclic substituted pyrimidines
US7557207B2 (en) 2004-11-24 2009-07-07 Rigel Pharmaceuticals, Inc. Spiro 2,4-pyrimidinediamine compounds and their uses
US8211929B2 (en) * 2004-12-30 2012-07-03 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
PT1856135E (en) 2005-01-19 2010-02-26 Rigel Pharmaceuticals Inc Prodrugs of 2,4-pyrimidinediamine compounds and their uses
US20060270694A1 (en) 2005-05-03 2006-11-30 Rigel Pharmaceuticals, Inc. JAK kinase inhibitors and their uses
WO2006129100A1 (en) * 2005-06-03 2006-12-07 Glaxo Group Limited Novel compounds
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
SG137989A1 (en) * 2005-06-08 2008-01-28 Rigel Pharmaceuticals Inc Compositions and methods for inhibition of the JAK pathway
CA2607901C (en) 2005-06-13 2016-08-16 Rigel Pharmaceuticals, Inc. Methods and compositions for treating degenerative bone disorders using a syk inhibitory 2,4-pyrimidinediamine
MX2008000574A (en) 2005-07-11 2008-03-14 Sanofi Aventis Novel 2,4-dianilinopyrimidine derivatives, the preparation thereof, their use as medicaments, pharmaceutical compositions and, in particular, as ikk inhibitors.
US8321953B2 (en) 2005-07-14 2012-11-27 Imation Corp. Secure storage device with offline code entry
WO2007053844A2 (en) 2005-10-31 2007-05-10 Rigel Pharmaceuticals, Inc. Compositions and methods for treating inflammatory disorders
MY167260A (en) 2005-11-01 2018-08-14 Targegen Inc Bi-aryl meta-pyrimidine inhibitors of kinases
US7713987B2 (en) 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
US7962290B1 (en) * 2006-01-09 2011-06-14 Rigel Pharmaceuticals, Inc. Identification of pharmacophores from co-crystals of spleen tyrosine kinase (SYK) and SYK ligands
WO2007085540A1 (en) 2006-01-27 2007-08-02 Glaxo Group Limited 1h-indaz0l-4-yl-2 , 4-pyrimidinediamine derivatives
SI1984357T1 (en) 2006-02-17 2014-02-28 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for treating or preventing autoimmune diseases
CA2642229C (en) 2006-02-24 2015-05-12 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
GB0605691D0 (en) 2006-03-21 2006-05-03 Novartis Ag Organic Compounds
CA2673125C (en) 2006-10-19 2015-04-21 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
CA2673137C (en) 2006-11-21 2015-02-10 Rigel Pharmaceuticals, Inc. Prodrug salts of 2,4-pyrimidinediamine compounds and their uses
US7947698B2 (en) 2007-03-23 2011-05-24 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
WO2008118823A2 (en) 2007-03-26 2008-10-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
WO2009003136A1 (en) 2007-06-26 2008-12-31 Rigel Pharmaceuticals, Inc. Substituted pyrimidine-2, 4 -diamines for treating cell proliferative disorders
CN101743009A (en) 2007-07-11 2010-06-16 辉瑞大药厂 Pharmaceutical compositions and methods of treating dry eye disorders
EP2183225A1 (en) 2007-07-17 2010-05-12 Rigel Pharmaceuticals, Inc. Cyclic amine substituted pyrimidinediamines as pkc inhibitors
PT2565193E (en) * 2009-01-23 2014-06-05 Rigel Pharmaceuticals Inc Compositions and methods for inhibition of the jak pathway

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001064654A1 (en) * 2000-03-01 2001-09-07 Astrazeneca Ab Pyrimidine compounds
WO2002004429A1 (en) * 2000-07-11 2002-01-17 Astrazeneca Ab Pyrimidine derivatives
WO2004041789A1 (en) * 2002-11-01 2004-05-21 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of jak and other protein kinases
WO2004041810A1 (en) * 2002-11-05 2004-05-21 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of jak and other protein kinases
WO2005012307A1 (en) * 2003-07-16 2005-02-10 Janssen Pharmaceutica N.V. Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors
WO2005012294A1 (en) * 2003-07-30 2005-02-10 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
WO2005013996A2 (en) * 2003-08-07 2005-02-17 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and uses as anti-proliferative agents
WO2005026130A1 (en) * 2003-09-18 2005-03-24 Novartis Ag 2,4-di (phenylamino) pyrimidines useful in the treatment of proliferative disorders
WO2006034872A1 (en) * 2004-09-29 2006-04-06 Bayer Schering Pharma Aktiengesellschaft Substituted 2-anilinopyrimidines as cell cycle kinase inhibitors or receptor tyrosine kinase inhibitors, production of said substances and use of the latter as medicaments

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of WO2006133426A2 *

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